FLUCONAZOLE : a medicine to treat fungal infections

Fluconazole is used to treat serious fungal or yeast infections, including vaginal candidiasis, oropharyngeal candidiasis (thrush, oral thrush), esophageal candidiasis (candida esophagitis), other candida infections (including urinary tract infections, peritonitis [inflammation of the lining of the stomach]

1. សាកលវិទ្យាល័យ​ អន្តរជាតិ INTERNATIONAL UNIVERSITY​ Fluconazole

2. Contents: Chemical Name Structure Mechanism of Action Mechanism of Resistance Indications Dosage Side Effects.

3. Chemical Name 01

4. 1. Chemical Name  2-(2,4-Difluorophenyl)-1,3-bis(1H-1,2,4-triazol-1-yl)propan-2-ol

5. Structure 02

6. 2. Structure  Fluconazole first generation synthesis triazole antifungal used to treat various fungal infections including candidiasis Molecular weight : 306.3g/mol

7. Mechanism of Action 03

8.   Mechanism of action inhibit the fungal cytochrome P-450 3-A dependent enzyme 14-alpha demethylase  interrupt the synthesis of ergosterol depletion of ergosterol in the cell membrane  accumulation of toxic intermediate sterols  increased membrane permeability inhibition of fungal growth

9. Mechanism of Resistance 04

10. 4. Mechanism of Resistance 1.The upregulation of drug efflux pump, primarily CDR1, CDR2 and MDR1 2.Mutational changes to 14-α-demethylase 3.Upregulation of ERG11 4.Other alterations to the cell's sterol pathway

11. Indications 05

12. 5. Indications Vaginal yeast infections caused by Candida Systemic Candida infections Both esophageal and oropharyngeal candidiasis Cryptococcal meningitis UTI (urinary tract infection) by Candida Peritonitis (inflammation of the peritoneum) caused by Candida

13. Dosage 06

14. 6. Dosage Vaginal candidiasis: 150mg/day.  Urinary tract infections or peritonitis: 50-200mg/day. Cryptococcal meningitis: 400mg for one day, followed by 200mg/day for at least 10-12 weeks. Esophageal candidiasis: 200mg for one day, followed by 100mg/day for at least three weeks.

15. Oropharyngeal candidiasis: 200mg for one day, followed by 100mg/day for at least two weeks. Other infections: Up to 400mg/day. Child dosing: The dose in children is determined by the physician based on child’s age and body weight.

16. Side Effects 07

17. 7. Side effects • GI -Dyspepsia -Vomiting -Taste disturbance • CNS -Dizziness -Seizures

18. •Liver -Hepatitis -Pruritus • Cardiac -QT prolongation -Torsades de pointes

19. • Skin -Alopecia -Skin rash -Toxic epidermal necrolysis -Stevens Johnson syndrome • Blood -Leukopenia -Thrombocytopenia

20. • Systemic/metabolic  - Hyperlipidaemia - Hypokalaemia - Hypersensitivity reactions -Anaphylaxis

21. Reference 08

22. https://journals.asm.org/doi/10.1128/aac.04613-14 https://go.drugbank.com/drugs/DB00196 Reference

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